AR073739A1 - Aminopirimidinas como inhibidores de los receptores de histamina - Google Patents
Aminopirimidinas como inhibidores de los receptores de histaminaInfo
- Publication number
- AR073739A1 AR073739A1 ARP090103486A ARP090103486A AR073739A1 AR 073739 A1 AR073739 A1 AR 073739A1 AR P090103486 A ARP090103486 A AR P090103486A AR P090103486 A ARP090103486 A AR P090103486A AR 073739 A1 AR073739 A1 AR 073739A1
- Authority
- AR
- Argentina
- Prior art keywords
- group
- heterocycloalkyl
- alkyl
- taken together
- heteroaryl
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0043—Nose
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Ophthalmology & Optometry (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos y métodos que pueden ser utiles como inhibidores de H1R y/o H4R para el tratamiento o la prevencion de enfermedades inflamatorias, autoinmunes, alergias, y oculares, composiciones farmacéuticas. Reivindicacion 1: Un método de tratamiento de una enfermedad mediada por H1R y/o H4R que comprende la administracion de una cantidad terapéuticamente efectiva de un compuesto de la formula estructural (1), o una de sus sales, en los cuales una línea de puntos indica que una union puede estar presente o ausente; X1 y X3 se seleccionan en forma independiente del grupo que consiste en [C(R2)(R3)] y NR4; X2 se selecciona del grupo que consiste en [C(R5)(R6)], NR7, O, y S; X4 se selecciona del grupo que consiste en [C(R8)(R9)], NR10, O, y S; X5 se selecciona del grupo que consiste en [C(R11)(R12)], NR13, O, y S; X6 se selecciona del grupo que consiste en [C(R14)(R15)], NR16, O, y S; X7 se selecciona del grupo que consiste en [C(R17)(R18)], NR19, O, S, y un enlace; X8 se selecciona del grupo que consiste en C y N; Y se selecciona del grupo que consiste en un enlace, NR1[C(R20)(R21)]n, NR1[C(R22)(R23)]n-W-(C(R24)(R25)]m, S-[C(R26)(R27)]n-W-[C(R28)(R29)]m, O[C(R30)(R31)]n, [C(R32)(R33)]n-W-[C(R34)(R35)]m, y [C(R36)(R37)]n; n y m son cada uno en forma independiente un numero entero desde 0 hasta 3; W se selecciona del grupo que consiste en O, S, S(O)2, NR38, NR39S(O2), C(O), C(S), C(O)O, C(O)NR40, NR41C(O), y NR42C(O)O; Z se selecciona del grupo que consiste en hidrogeno, arilo, alquilo, heterocicloalquilo, y cicloalquilo, cualquiera de los cuales puede estar sustituido en forma opcional; R1 hasta R42 se selecciona cada uno en forma independiente del grupo que consiste en nulo, hidrogeno, alquilo, heteroalquilo, alcoxi, halogeno, haloalquilo amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, mercaptilo, alquilsulfonilo, sulfonamida, y alquilsulfonamido, cualquiera de los cuales puede estar sustituido en forma opcional; o R11 y R14, tomados juntos, forman un cicloalquilo parcialmente saturado, o R1 y R20, tomados juntos, forman un heterocicloalquilo; o R1 y R22, tomados juntos, forman un heterocicloalquilo; o R22 y R38, tomados juntos, forman un heterocicloalquilo; o R1 y R38, tomados juntos, forman un heterocicloalquilo. Reivindicacion 42: Un compuesto, para usar en la fabricacion de un medicamento para la prevencion o el tratamiento de una enfermedad o afeccion aliviada por la inhibicion de H1R y/o H4R, de la formula estructural (2), o una de sus sales, en los cuales: X1 se selecciona del grupo que consiste en [C(R2)] y N; Y se selecciona del grupo que consiste en un enlace, NR1[C(R20)(R21)]n, NR1[C(R22)(R23)]n-W-[C(R24)(R25)]m, S-[C(R26)(R27)]n-W-[C(R28)(R29)]m, O[C(R30)(R31)]n, [C(R32)(R33)]n-W-[C(R34)(R35)]m, y [C(R36)(R37)]n; n y m son cada uno en forma independiente un numero entero desde 0 hasta 3; W se selecciona del grupo que consiste en O, S, S(O)2, NR38, NR39S(O2), C(O), C(S), C(O)O, C(O)NR40, NR41C(O)O, y NR42C(O)O; Z se selecciona del grupo que consiste en arilo, alquilo, heterocicloalquilo, alcoxicarbonilo, acilo, y cicloalquilo, cualquiera de los cuales puede estar sustituido en forma opcional, R1, R2, R14 y R20 hasta R42 se selecciona cada uno en forma independiente del grupo que consiste en hidrogeno, alquilo, heteroalquilo, alcoxi, halogeno, haloalquilo, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, mercaptilo, alquilsulfonilo, sulfonamida, y alquilsulfonamido, cualquiera de los cuales puede estar sustituido en forma opcional; o R11 y R14, tomados juntos, forman un cicloalquilo parcialmente saturado; o R1 y R20, tomados juntos, forman un heterocicloalquilo, o R1 y R22, tomados juntos, forman un heterocicloalquilo; o R22 y R38, tomados juntos, forman un heterocicloalquilo; o R1 y R38, tomados juntos, forman un heterocicloalquilo; R11 se selecciona del grupo que consiste en hidrogeno, alquilo, heteroalquilo, alcoxi, halogeno, haloalquilo, amino, aminoalquilo, amido, carboxilo, acilo, hidroxi, ciano, nitro, arilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo, heterocicloalquilalquilo, heteroarilo, heteroarilalquilo, mercaptilo, alquilsulfonilo, sulfonamida, y alquilsulfonamido, cualquiera de los cuales puede estar sustituido en forma opcional; y con las salvedades de que: si Y es NR1[C(R20)(R21)]n, R1 es hidrogeno, y n es 0, entonces Z no es arilo o heteroarilo; y si Y es NR1[C(R22)(R23)]n-W-[C(R24)(R25)]m, n es 2, m es 0, W es NR38, R22, y R23 son hidrogeno, y R1 y R38, tomados juntos, forman un anillo de piperazina, entonces Z no es fenilo o metilo.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US9581908P | 2008-09-10 | 2008-09-10 |
Publications (1)
Publication Number | Publication Date |
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AR073739A1 true AR073739A1 (es) | 2010-12-01 |
Family
ID=41799808
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP090103486A AR073739A1 (es) | 2008-09-10 | 2009-09-10 | Aminopirimidinas como inhibidores de los receptores de histamina |
Country Status (12)
Country | Link |
---|---|
US (1) | US20100063047A1 (es) |
EP (1) | EP2320904A4 (es) |
JP (1) | JP2012502104A (es) |
KR (1) | KR20110092267A (es) |
CN (1) | CN102186479A (es) |
AR (1) | AR073739A1 (es) |
AU (1) | AU2009291783A1 (es) |
CA (1) | CA2735368A1 (es) |
MX (1) | MX2011002263A (es) |
TW (1) | TW201024307A (es) |
UY (1) | UY32110A (es) |
WO (1) | WO2010030757A2 (es) |
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AU2010289321A1 (en) | 2009-09-04 | 2012-04-05 | The Regents Of The University Of Michigan | Compositions and methods for treatment of leukemia |
AU2010339444A1 (en) * | 2009-12-30 | 2012-07-19 | Arqule, Inc. | Substituted pyrrolo-aminopyrimidine compounds |
TW201200518A (en) | 2010-03-10 | 2012-01-01 | Kalypsys Inc | Heterocyclic inhibitors of histamine receptors for the treatment of disease |
TR201002256A1 (tr) * | 2010-03-24 | 2011-10-21 | Sanovel �La� Sanay� Ve T�Caret Anon�M ��Rket� | Stabil aliskiren formülasyonları |
TW201206936A (en) * | 2010-07-19 | 2012-02-16 | Alcon Res Ltd | Methods and compositions for the treatment of allergy |
WO2012044993A1 (en) * | 2010-09-30 | 2012-04-05 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Compounds, pharmaceutical compositions, and methods of treating or preventing neurodegenerative diseases or disorders |
WO2012068390A1 (en) * | 2010-11-17 | 2012-05-24 | The Curators Of The University Of Missouri | INHIBITORS OF FOOT AND MOUTH DISEASE VIRUS TARGETING THE RNA-DEPENDENT POLYMERASE ACTIVITY OF 3Dpol |
US8980924B2 (en) | 2010-11-24 | 2015-03-17 | The Trustees Of Columbia University In The City Of New York | Non-retinoid RBP4 antagonist for treatment of age-related macular degeneration and stargardt disease |
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PE20080371A1 (es) * | 2006-05-19 | 2008-04-09 | Wyeth Corp | N-benzoil-y-n-bencilpirrolidin-3-ilaminas como antagonistas de histamina-3 |
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- 2009-09-10 CA CA2735368A patent/CA2735368A1/en not_active Abandoned
- 2009-09-10 US US12/556,842 patent/US20100063047A1/en not_active Abandoned
- 2009-09-10 JP JP2011526965A patent/JP2012502104A/ja active Pending
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CN102186479A (zh) | 2011-09-14 |
JP2012502104A (ja) | 2012-01-26 |
AU2009291783A1 (en) | 2010-03-18 |
EP2320904A4 (en) | 2011-09-14 |
TW201024307A (en) | 2010-07-01 |
WO2010030757A2 (en) | 2010-03-18 |
MX2011002263A (es) | 2011-05-23 |
CA2735368A1 (en) | 2010-03-18 |
KR20110092267A (ko) | 2011-08-17 |
WO2010030757A3 (en) | 2010-09-02 |
EP2320904A2 (en) | 2011-05-18 |
US20100063047A1 (en) | 2010-03-11 |
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